A JAK1 inhibitor
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Abrocitinib

Item No. 34869

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[cis-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)cyclobutyl]-1-propanesulfonamide
CAS Number
1622902-68-4
Synonyms
  • PF-04965842
Molecular Formula
C14H21N5O2S
Formula Weight
323.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
288 nm
SMILES
CN([C@H]1C[C@H](C1)NS(CCC)(=O)=O)C2=C3C(NC=C3)=NC=N2
InChi Code
InChI=1S/C14H21N5O2S/c1-3-6-22(20,21)18-10-7-11(8-10)19(2)14-12-4-5-15-13(12)16-9-17-14/h4-5,9-11,18H,3,6-8H2,1-2H3,(H,15,16,17)/t10-,11+
InChi Key
IUEWXNHSKRWHDY-PHIMTYICSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $79

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    10 mg

    $134

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    25 mg

    $237

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    50 mg

    $316

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    Product Description

    Abrocitinib is a JAK1 inhibitor (IC50 = 0.029 µM).1 It is selective for JAK1 over JAK2, JAK3, and TYK2 (IC50s = 0.803, >10, and 1.253 µM, respectively) and a panel of 40 kinases at 1 µM. Abrocitinib inhibits IFN-α-, IL-21-, or IL-27-induced phosphorylation of STAT3 (IC50s = 0.189, 0.511, and 0.271 µM, respectively) and IFN-γ-induced phosphorylation of STAT1 (IC50 = 0.163 µM) in isolated human whole blood. It reduces paw edema in a rat model of adjuvant-induced arthritis when administered at doses of 1, 5, and 15 mg/kg. Formulations containing abrocitinib have been used in the treatment of atopic dermatitis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Vazquez, M.L., Kaila, N., Strohbach, J.W., et al. Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A selective JAK1 clinical candidate for the treatment of autoimmune diseases. J. Med. Chem. 61(3), 1130-1152 (2018).